Dendrimers comprised of heterogeneous polymeric segments (e.g., hydrophobic and hydrophilic) afford multiple properties in a single molecule. Such dendrimers are described as “Janus type” and can be obtained by coupling two dendrons—possessing chemically different properties—to a single core. A unique property exhibited by these Janus dendrimers is the formation of various types of nanoparticles in aqueous media, depending on the ratio between the heterogeneous polymeric segments. However, lack of synthetic feasibility has hindered the widespread adoption of Janus dendrimers in drug delivery literature. In addition, they suffer from poor solubility and cytotoxicity—limiting clinical application. Alternatively, linear-dendritic block copolymers (LDBCs) combine the advantageous properties of dendritic polymers with that of linear copolymers to afford nanomaterials with superior mechanical properties. Herein, we report the analysis of a library of polymers analogous to Janus dendrimers, known as Janus linear-dendritic hybrids composed of a hydrophilic polyamidoamine (PAMAM) dendron covalently linked to a hydrophobic polyester. This combines the advantages regarding drug uptake and release of dendritic systems with the synthetic accessibility and precise molecular weight control of traditional polymerization techniques. Within the study, heterobifunctional groups were incorporated at the hydrophilic block to investigate the interfacial behavior of the nanoparticle surface and towards providing several biological advantages such as efficient cell penetrating ability. In conjunction with microscopy (e.g., TEM and AFM), spectroscopic and light scattering techniques afford evidence of nanoparticle formation. The mean diameters of the nanoparticles formulated at concentrations of 1-10 mg/mL ranged between 30-300 nm. The size of the nanoparticles depend on the formulation method employed. Results of the study suggest materials applicable as next generation drug delivery systems.

PAMAM-polylactide, “Janus-type” hybrids as next-generation biomaterials

2019 Spring National Meeting

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